PF 429242 dihydrochloride

Pricing Availability   Qty
Description: Competitive inhibitor of SREBP site 1 protease
Chemical Name: 4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide dihydrochloride
Purity: ≥97% (HPLC)
Citations (6)
Literature (1)
Pathways (1)

Biological Activity for PF 429242 dihydrochloride

PF 429242 dihydrochloride is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 μM). Also displays antiviral activity. Cell permeable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 429242 dihydrochloride

PF 429242 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 429242 dihydrochloride

M. Wt 482.49
Formula C25H35N3O2.2HCl
Storage Desiccate at RT
Purity ≥97% (HPLC)
CAS Number 2248666-66-0
PubChem ID 90488837
Smiles O=C(C2=CC=C(CN(CC)CC)C=C2)N(CCC3=CC=CC=C3OC)[C@@H]1CCNC1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 429242 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 24.12 50
DMSO 24.12 50

Preparing Stock Solutions for PF 429242 dihydrochloride

The following data is based on the product molecular weight 482.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.15 mL 20.73 mL 41.45 mL
2.5 mM 0.83 mL 4.15 mL 8.29 mL
5 mM 0.41 mL 2.07 mL 4.15 mL
25 mM 0.08 mL 0.41 mL 0.83 mL

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Product Datasheets for PF 429242 dihydrochloride

Certificate of Analysis / Product Datasheet
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References for PF 429242 dihydrochloride

References are publications that support the biological activity of the product.

Hay et al (2007) Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg.Med.Chem.Lett. 17 4411 PMID: 17583500

Hawkins et al (2008) Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J.Pharmacol.Exp.Ther. 326 801 PMID: 18577702

Urata et al (2011) Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J.Virol. 85 795 PMID: 21068251

Olmstead (2012) Human subtilase SKI-1/S1P is a master regulator of the HCV lifecycle and a potential host cell target for developing indirect-acting antiviral agents. PLoS.Pathog. 8 e1002468 PMID: 22241994

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Keywords: PF 429242 dihydrochloride, PF 429242 dihydrochloride supplier, SREBP, sterol, regulatory, element, binding, proteins, inhibitors, inhibits, site, 1, proteases, S1P, serine, antivirals, PF429242, Other, Proteases, Non-selective, Antivirals, 3354, Tocris Bioscience

6 Citations for PF 429242 dihydrochloride

Citations are publications that use Tocris products. Selected citations for PF 429242 dihydrochloride include:

Scott et al (2018) TFAP2 transcription factors are regulators of lipid droplet biogenesis. Elife 7 PMID: 30256193

Uchida et al (2016) Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation. Viruses 8 E46 PMID: 26875984

Kleinfelter et al (2015) Haploid Genetic Screen Reveals a Profound and Direct Dependence on Cholesterol for Hantavirus Membrane Fusion. Ann Rheum Dis 6 e00801 PMID: 26126854

Tien et al (2019) Ambient particulate matter attenuates Sirtuin1 and augments SREBP1-PIR axis to induce human pulmonary fibroblast inflammation: molecular mechanism of microenvironment associated with COPD. Aging (Albany NY) 11 4654 PMID: 31299012

Do you know of a great paper that uses PF 429242 dihydrochloride from Tocris? Please let us know.

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Literature in this Area

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Cancer Metabolism Poster

Cancer Metabolism Poster

This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.

Pathways for PF 429242 dihydrochloride

Insulin Signaling Pathway

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.